CPI-203 CAS:1446144-04-2, a primary amide analog of (+)-JQ1, is a potent, selective and competitive small molecule inhibitor of BET bromodomain with an average GI50 value of 0.23μM in MCL cell lines . It exhibits excellent bioavailability when administered orally or intraperitoneally. CPI-203 downregulates Myc expression, causes G1 cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. As an inhibitor of BET protein, CPI-203 inhibits BRD4 in vitro and in cells. It inhibits specific Ser2 phosphorylation of endogenous BRD4 and exogenous mutant BRD4 (BRD4 FEE-AAA) in vivo, thereby blocking BRD4 recruitment to chromatin.
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